植物来源的生物碱类乙酰胆碱酯酶抑制剂研究进展_孙春红.pdf

·3172· 中草药 Chinese Traditional and Herbal Drugs 第 45 卷 第 21 期 2014 年 11 月 ·综 述· 植物来源的生物碱类乙酰胆碱酯酶抑制剂研究进展 孙春红，邹峥嵘* 江西师范大学生命科学学院 江西省亚热带植物资源保护与利用重点实验室，江西 南昌 330022 摘 要：乙酰胆碱酯酶抑制剂是阿尔茨海默病治疗药物的研究热点。根据类胆碱学说，乙酰胆碱酯酶抑制剂可提高脑部神经 递质乙酰胆碱的水平从而改善阿尔茨海默病患者的胆碱功能，并缓解神经性紊乱的症状。植物天然产物是乙酰胆碱酯酶抑制 剂先导化合物的重要来源，其中生物碱为此类天然产物的重要组成部分。综述植物来源且具有抗乙酰胆碱酯酶活性生物碱的 结构类型、作用机制及其构效关系。 关键词：乙酰胆碱酯酶抑制剂；生物碱；天然产物；药用植物；阿尔茨海默病 中图分类号：R284；R285 文献标志码：A 文章编号：0253 - 2670(2014)21 - 3172 - 13 DOI: 10.7501/j.issn.0253-2670.2014.21.024 Research progress on plant-derived acetylcholinesterase inhibitory alkaloids SUN Chun-hong, ZOU Zheng-rong Key Laboratory of Protection and Utilization of Subtropic Plant Resources of Jiangxi Province, Jiangxi Normal University, Nanchang 330022, China Abstract: Acetylcholinesterase (AChE) inhibitor is a research hotspot in the treatment of Alzheimer’s disease (AD). According to the cholinergic hypothesis, the AChE inhibitors can increase the level of neurotransmitter acetylcholine in the brain, thus improving cholinergic functions in patients with AD and alleviating the symptoms of this neurological disorder. As AChE inhibitor is an important therapeutic strategy for AD, efforts are being made in the search for new molecules with anti-AChE activity. The fact that naturally-occurring compounds from plants are considered to be a potential source of new inhibitors has led to the discovery of an important number of AChE inhibitory alkaloids. Since the approval of galantamine for the treatment of AD patients, the search for new anticholinesterase alkaloids has escalated. This review summarizes recent advances in current knowledge on alkaloids as AChE inhibitors, and outlines the structure-activity relationship and docking studies. Key words: acetylcholinesterase inhibitors; alkaloids; na